Identification, Optimization and Structural Investigation of Antiprotozoal Agents and Molecular Target

Neglected and emerging tropical diseases caused by eukaryotic pathogens impact hundreds of millions of people worldwide. These diseases are primarily endemic to Asia, the Middle East, Africa, and South and Central America, yet they also pose a significant threat to global public health, including within the United States. Continued efforts to control, eliminate, and provide safe and effective treatment options remain critical.

A series of chemical entities has been identified to serve as templates for further discovery and development. This project will employ a combination of structure-based and natural products–based drug discovery approaches. Additionally, the molecular interactions between the cysteine protease drug target from Trypanosoma brucei and its inhibitors will be structurally characterized.

The successful execution of the project’s aims and objectives will contribute to the understanding of structural chemotypes important for antitrypanosomal and antimalarial drug discovery. Furthermore, it will help expand the drug development pipeline for Human African Trypanosomiasis (HAT) and Leishmaniasis.

NIH Project details

Basic Science
Drug-based Strategies
Enabling Technologies & Assays

Sep 2017 — Jun 2021

$453,000

United States